کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10587663 | 981431 | 2013 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery of thiazolyl-phthalazinone acetamides as potent glucose uptake activators via high-throughput screening
ترجمه فارسی عنوان
کشف تیازولیل فتالازینون استامید به عنوان فعال کننده های جذب گلوکز با استفاده از غربالگری بالا
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
چکیده انگلیسی
With the aim to discover orally active small molecules that stimulate glucose uptake, high throughput screening of a library of 5000 drug-like compounds was conducted in differentiated skeletal muscle cells in presence of insulin. N-Substituted phthalazinone acetamide was identified as a potential glucose uptake modulator. Several novel derivatives were synthesized to establish structure activity relationships. Identified lead thiazolyl-phthalazinone acetamide (7114863) increased glucose uptake (EC50 of 0.07 ± 0.02 μM) in differentiated skeletal muscle cells in presence of insulin. Furthermore, 7114863 was superior to rosiglitazone under similar experimental conditions without inducing PPAR-γ agonist activity thus making it a very interesting scaffold.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 20, 15 October 2013, Pages 5740-5743
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 20, 15 October 2013, Pages 5740-5743
نویسندگان
Madhavi Agrawal, Prashant Kharkar, Sonali Moghe, Tushar Mahajan, Vaishali Deka, Chandni Thakkar, Amrutha Nair, Chirag Mehta, Julie Bose, Asha Kulkarni-Almeida, Dilip Bhedi, Ram A. Vishwakarma,